drug

Ascorbic acid, rutoside drug combination is used for treating diabetic retinopathy.

PKG drug G1 targets PKG Iα C42. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.

Puxitatug samrotecan drug-linker (AZD8205 drug-linker), comprising a degradable ADC linker and the topoisomerase I inhibitor Exatecan, is utilized in the ADC (drug-linker conjugate for ADC) targeting the anti-B7-H4 antibody.

Cisplatin (CDDP) is a chemotherapeutic agent with antitumor activity and is a classic DNA crosslinker. It inhibits DNA synthesis and induces DNA damage in cancer cells by forming DNA adducts, ultimately leading to cell death. In addition, Cisplatin can activate ferroptosis and induce autophagy. In animal studies, it is commonly used to establish models of chronic kidney injury and acute renal failure.

PD 198306 is a selective inhibitor of MAPK/ERK-kinase (MEK) with antihyperalgesic effects. PD 198306 reduces the Streptozocin-induced increase in the level of active ERK1.

Bamaquimast (L 0042) is a proton pump inhibitor for the study of asthma-like immune system disorders and respiratory diseases.

N-Acetylcarnosine (N-Acetyl-L-carnosine) is thought to be able to combat some of the effects of oxidative stress as it has anti-oxidant properties.

Cetaben, a PPARα-independent peroxisome proliferator, is a non-fibrotic lipid-lowering drug that effectively reduces cholesterol and triglyceride concentrations.

G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.

Dobutamine hydrochloride (Dobutamine (hydrochloride)) is a catecholamine that acts as a β-adrenergic receptor agonist with potent positive inotropic effects.

SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor with IC50 of 0.1-1.8 μM. It induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1.

Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and a maleimide-GGFG peptide linker used in the synthesis of DS-8201 and U3-1402.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

4-Hydroxymephenytoin ((+/-)-4'-Hydroxymephenytoin) is the metabolism of an antiepileptic drug mephenytoin. Mephenytoin is used as a CYP2C19 substrate.

Didesethyl chloroquine (Bisdesethylchloroquine) is an effective myocardial inhibitor. Didesethyl chloroquine (Bisdesethylchloroquine) is the main metabolite of the antimalarial drug chloroquine.

Allopurinol riboside is a metabolite of allopurinol with potency against parasites. Allopurinol riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a Ki of 277 μM.

Methotrexate metabolite (DAMPA) (DAMPA) is the active metabolite of Methotrexate. Methotrexate is a folic acid antagonist. Methotrexate is used as a chemotherapeutic agent and immunosuppressant.

LGE-899 (Sonidegib metabolite M48) is a main metabolite of Sonidegib which is an inhibitor of the hedgehog pathway. The Tmax of LGE-899(60 h) is much longer than Sonidegib.

Inz-1 is an effective and fungal-selective inhibitor of mitochondrial cytochrome bc1 with IC50s of 8.092 and 45.320 μM for yeast and human. Inz-1 reverses Fluconazole or other triazole antifungals' resistance in the pathogenic fungus Candida albicans.

Vedaprofen (PM 150) inhibits COX-1 and reduces prostaglandin H2 synthesis with anti-inflammatory activities. Vedaprofen is an inhibitor of Escherichia coli sliding clamp with the IC50 of 222 μM and Ki of 131 μM.

DP-1 hydrochloride is a degradation product of SDC-TRAP-0063, a fragment of Ganetespib, a heat shock protein 90 (HSP90) inhibitor with antitumor activity.

GS-829845 is a JAK1 inhibitor, the main component of the active metabolite of Filgotinib, which is approximately 10-fold less potent and has a longer half-life than the parent.

Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research.

2-Hydroxy atorvastatin calcium salt is a hydroxy metabolite of atorvastatin calcium salt, a potent HMG-CoA reductase inhibitor (IC50 = 8 nM).